CYM-5520

Cas No.:	1449747-00-5
Chemical Name:	CYM-5520
Synonyms:	CYM-5520;CYM 5520;CYM5520
SMILES:	N#CC(C=C1)=CN(CC(C2=C(C)N(CC3=CC=CC=C3)C(C)=C2)=O)C1=O
Formula:	C21H19N3O2
M.Wt:	345.39
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	CYM-5520 is a selective and allosteric sphingosine 1-phosphate receptor 2 (S1PR2) agonist with an EC50 of 480 nM. CYM-5520 does not activate S1PR1, S1PR3, S1PR4 and S1PR5 receptors. CYM-5520 can co-bind in the S1PR2 receptor with S1P. CYM-5520 can be used for osteoporosis research[1][2].
In Vivo:	CYM-5520 (10 mg/kg; i.p.; 5 consecutive days per week; for 6 weeks) treatment clearly increases long bone and vertebral bone mass in osteopenic ovariectomized mice. CYM-5520 also increases osteoblast number, osteoid surface and alkaline phosphatase, and plasma concentrations of the osteoanabolic marker procollagen I C-terminal propeptide are also elevated[2]. Animal Model: Ovariectomized 12 weeks old C57Bl6J mice[2] Dosage: 10 mg/kg Administration: i.p.; 5 consecutive days per week; for 6 weeks Result: Corrected ovariectomy-induced osteopenia in mice by inducing new bone formation.
In Vitro:	CYM-5520 (EC50 of 1.6 μM) is a full agonist for wild type S1PR2. Stimulation of cells expressing the triple mutant S1PR2 with S1P does not elicit a rise in luciferase activity, whereas the CYM-5520 is an agonist with an EC50 of 1.5 μM[1].
References:	[1]. Hideo Satsu, et al. A sphingosine 1-phosphate receptor 2 selective allosteric agonist. Bioorg Med Chem. 2013 Sep 1;21(17):5373-82. [2]. Sarah Weske, et al. Agonist-induced activation of the S1P receptor 2 constitutes a novel osteoanabolic therapy for the treatment of osteoporosis in mice. Bone. 2019 Aug;125:1-7.